Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position

As part of the structure-activity relationship study undertaken around the pyrido[3,4-g]quinazoline moiety, new derivatives substituted at the 8-position were synthesized and evaluated regarding their ability to inhibit various protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3). Most active compound ex...

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Bibliographic Details
Published in:ARKIVOC free online journal of organic chemistry 2020-07, Vol.2020 (7), p.105-116
Main Authors: Esvan, Yannick J., Josselin, Béatrice, Baratte, Blandine, Bach, Stéphane, Ruchaud, Sandrine, Anizon, Fabrice, Giraud, Francis, Moreau, Pascale
Format: Article
Language:English
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Chemical Sciences
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Summary:As part of the structure-activity relationship study undertaken around the pyrido[3,4-g]quinazoline moiety, new derivatives substituted at the 8-position were synthesized and evaluated regarding their ability to inhibit various protein kinases (CDK5, CLK1, DYRK1A, CK1, GSK3). Most active compound exhibited a nanomolar potency toward CLK1, demonstrating that substitution at 8-position is compatible with CLK1 inhibition.
ISSN:1551-7012
1551-7004
1551-7012
DOI:10.24820/ark.5550190.p011.268